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Resveratrol sustained-release preparation and preparation method thereof

A resveratrol, slow-release preparation technology, applied in the field of sustainable release of free resveratrol preparations, can solve the problems of low resveratrol content, complex process, low resveratrol, etc., to improve biological Utilization, simple preparation process, and the effect of reducing the number of times of taking

Active Publication Date: 2022-07-12
INNOBIO CORP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the content of resveratrol in the granules is less than 30%, which is relatively low, and the relevant release results have not been provided, and the problem of human body absorption and utilization has not been solved
This product improves the stability of resveratrol and contains 1-2h release results, but the content of resveratrol is low, the process is complicated, and the use of organic solvents and pharmaceutical excipients limits the application of the product
[0006] CN101703479A discloses a resveratrol pellet and a preparation method thereof. Resveratrol is added to an excipient, pulverized to a micronized level, and mixed; the adhesive is dissolved in water, absolute ethanol or hydrous ethanol In the solution; using pellet forming technology such as pan-pellet method, extrusion-spheronization pelleting method or centrifugal-fluidized pelletizing method to make pellets, the content of resveratrol in this product is low, organic solvent is used, and medicinal Excipients, subsequent coating needs to be continued to achieve the sustained release effect, and the application of complex products is limited
[0007] Although the above-mentioned existing records involve improving the stability of resveratrol, some of which involve the release data of resveratrol, the content of resveratrol is low, and the release rate is generally only 1-2h slow-release effect, lacking long-term release ability, Moreover, there are still disadvantages such as complex production process, use of organic solvents and pharmaceutical excipients, and the product application is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Slow-release resveratrol granules A and its evaluation

[0023] (1) drop microcrystalline cellulose 80g, hydroxypropyl methylcellulose (viscosity 15mpa.s) 8g into 300ml water to prepare a uniform emulsion, take by weighing 910g of resveratrol 98% raw material powder and mix and stir to prepare Mixture I;

[0024] (2) mixture 1 is poured into high shear granulator for granulation, stirring speed 2000rpm, cutter speed 2500rpm, 2min, adopts 30 mesh sieves to granulate to make resveratrol granules.

[0025] (3) The resveratrol particles are placed in a fluidized bed with an inlet air temperature of 55°C and an air volume of 35m 3 Slow-release resveratrol granules A were obtained by thermal drying for about 1 hour per hour.

[0026] The sustained-release resveratrol granules A were prepared according to the above process, and the particle size was 0.3-0.6mm-like spherical granules, and the content detected by Agilent 1260 high performance liquid chromatography was...

Embodiment 2

[0031] Example 2 Slow-release resveratrol granules B and its evaluation

[0032] (1) drop microcrystalline cellulose 80g, hydroxypropyl methylcellulose (viscosity 5mpa.s) 8g into 360ml water to prepare a uniform emulsion, take by weighing 910g of resveratrol 98% raw material powder and mix and stir to prepare Mixture I;

[0033] (2) mixture 1 is poured into high shear granulator for granulation, stirring speed 2000rpm, cutter speed 2500rpm, 2min, adopts 30 mesh sieves to granulate to make resveratrol granules.

[0034] (3) The resveratrol particles are placed in a fluidized bed with an inlet air temperature of 55°C and an air volume of 35m 3 Slow-release resveratrol granules B were obtained by thermal drying for about 1 hour per hour.

[0035] The sustained-release resveratrol granules B were prepared according to the above process, with a particle size of 0.3-0.6mm spherical granules, and the content detected by Agilent 1260 high performance liquid chromatography was 88.9%; ...

Embodiment 3

[0037] Example 3 Slow-release resveratrol granules C and its evaluation

[0038] (1) drop microcrystalline cellulose 80g, hydroxypropyl methylcellulose (viscosity 50mpa.s) 8g into 400ml water to prepare a uniform emulsion, take by weighing 910g of resveratrol 98% raw material powder and mix and stir to prepare Mixture I;

[0039] (2) mixture 1 is poured into high shear granulator for granulation, stirring speed 2000rpm, cutter speed 2500rpm, 2min, adopts 30 mesh sieves to granulate to make resveratrol granules.

[0040] (3) The resveratrol particles are placed in a fluidized bed with an inlet air temperature of 55°C and an air volume of 35m 3 Slow-release resveratrol granules B were obtained by thermal drying for about 1 hour per hour.

[0041] The sustained-release resveratrol granules C were prepared according to the above process, and the particle size was 0.3-0.6mm spherical granules, and the content was 89.9% detected by Agilent 1260 high performance liquid chromatograph...

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PUM

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Abstract

The invention discloses a resveratrol sustained-release preparation and a preparation method thereof. The preparation method includes the steps of granulating and drying mixed raw materials, wherein the mixed raw materials contain resveratrol, excipients, viscosity mixture and water; the excipient is selected from microcrystalline cellulose, lactose and pregelatinized starch. The resveratrol preparation prepared by the invention has a resveratrol content of 10% to 95%; the appearance is spherical or quasi-spherical, the particle size is 0.3 to 0.6 mm, and the product has excellent fluidity; it is suitable for capsules and tablets. or in solid beverage form. In addition, the preparation process of the method of the invention is simple, the formula adopts food-grade excipients, does not use organic solvents, improves the stability of resveratrol, slowly releases the resveratrol after the human body takes it to maintain the peak blood concentration, reduces the number of taking times, and improves the bioavailability. Spend.

Description

technical field [0001] The present application relates to a dietary supplement, in particular to a formulation with a high content of sustainably releasing free resveratrol. Background technique [0002] The chemical name of resveratrol is (E)-3,5,4-trihydroxystilbene, which is a non-flavonoid polyphenolic compound. Resveratrol is insoluble in water, and the solubility in water is 30mg / L. Resveratrol is unstable to light and exists in free state and glycoside under natural conditions, with cis and trans isomers, respectively. Resveratrol mainly exists in the trans form in plants, and the physiological activity of the trans isomer is stronger than that of the cis isomer. [0003] Resveratrol exists in a variety of human foods such as mulberries, peanuts, pineapples, and grapes, and has high safety. Studies have shown that resveratrol has a variety of pharmacological activities, such as inhibiting cell proliferation, antioxidant, anti-inflammatory, antibacterial and antivir...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A23L33/00
CPCA23L33/00A23V2002/00A23V2200/30
Inventor 李向成陈剑彬吕福臻吴文忠
Owner INNOBIO CORP LTD